2012Current Drug MetabolismRequires access

Utility of Assessing Thiopurine S-methyltransferase Polymorphisms Before Azathioprine Therapy

Teresa Cabaleiro, Manuel Román, Javier P. Gisbert, Francisco Abad‐Santos

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Abstract

Thiopurine S-methyltransferase (TPMT) catalyzes the methylation of thiopurine drugs, such as azathioprine and mercaptopurine, which are used in a variety of diseases. Several mutations in the TPMT gene correlate with low enzyme activity and subsequent adverse effects, mainly myelotoxicity. Hence, genotyping TPMT makes it possible to identify patients at high risk of drug toxicity and adjust dosage accordingly. However, further research about the availability of a reliable and universal screening method and more costeffectiveness studies are necessary.

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What this paper is about

Thiopurine S-methyltransferase (TPMT) catalyzes the methylation of thiopurine drugs, such as azathioprine and mercaptopurine, which are used in a variety of diseases. Several mutations in the TPMT gene correlate with low enzyme activity and subsequent adverse effects, mainly myelotoxicity. Hence, genotyping TPMT makes it possible to identify patients at high risk of drug toxicity and adjust dosage accordingly. However, further research about the availability of a reliable and universal screening method and more costeffectiveness studies are necessary.

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Available abstract

Thiopurine S-methyltransferase (TPMT) catalyzes the methylation of thiopurine drugs, such as azathioprine and mercaptopurine, which are used in a variety of diseases. Several mutations in the TPMT gene correlate with low enzyme activity and subsequent adverse effects, mainly myelotoxicity. Hence, genotyping TPMT makes it possible to identify patients at high risk of drug toxicity and adjust dosage accordingly. However, further research about the availability of a reliable and universal screening method and more costeffectiveness studies are necessary.

Key concepts: Thiopurine methyltransferase, Azathioprine, Methyltransferase, Genotyping, Pharmacogenetics, Pharmacology, Medicine, Adverse effect

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